Hemab Therapeutics, Copenhagen, Denmark.
Center for Benign Haematology, Thrombosis and Haemostasis, Van Creveldkliniek, University Medical Center Utrecht, Utrecht University, Utrecht, Netherlands.
Nat Cardiovasc Res. 2024 Feb;3(2):166-185. doi: 10.1038/s44161-023-00418-4. Epub 2024 Feb 8.
Inherited bleeding disorders such as Glanzmann thrombasthenia (GT) lack prophylactic treatment options. As a result, serious bleeding episodes are treated acutely with blood product transfusions or frequent, repeated intravenous administration of recombinant activated coagulation factor VII (rFVIIa). Here we describe HMB-001, a bispecific antibody designed to bind and accumulate endogenous FVIIa and deliver it to sites of vascular injury by targeting it to the TREM (triggering receptor expressed on myeloid cells)-like transcript-1 (TLT-1) receptor that is selectively expressed on activated platelets. In healthy nonhuman primates, HMB-001 prolonged the half-life of endogenous FVIIa, resulting in its accumulation. Mouse bleeding studies confirmed antibody-mediated potentiation of FVIIa hemostatic activity by TLT-1 targeting. In ex vivo models of GT, HMB-001 localized FVIIa on activated platelets and potentiated fibrin-dependent platelet aggregation. Taken together, these results indicate that HMB-001 has the potential to offer subcutaneous prophylactic treatment to prevent bleeds in people with GT and other inherited bleeding disorders, with a low-frequency dosing regimen.
遗传性出血性疾病,如 Glanzmann 血小板无力症(GT)缺乏预防性治疗选择。因此,严重的出血发作通过输注血液制品或频繁、重复地静脉内给予重组激活凝血因子 VII(rFVIIa)进行急性治疗。在这里,我们描述了 HMB-001,这是一种双特异性抗体,旨在通过靶向表达于激活血小板上的 TREM(髓样细胞表达的触发受体)样转录物-1(TLT-1)受体来结合和积累内源性 FVIIa,并将其递送至血管损伤部位。在健康的非人类灵长类动物中,HMB-001 延长了内源性 FVIIa 的半衰期,导致其积累。小鼠出血研究证实了 TLT-1 靶向对 FVIIa 止血活性的抗体介导增强作用。在 GT 的体外模型中,HMB-001 将 FVIIa 定位在激活的血小板上,并增强了纤维蛋白依赖性血小板聚集。综上所述,这些结果表明,HMB-001 有可能提供皮下预防性治疗,以预防 GT 和其他遗传性出血性疾病患者的出血,具有低频率的给药方案。